Cholesteryl Cytofectins with Primary Amino Head Groups Transfect Transformed Human Epithelial Cell Lines Efficiently

Two novel cholesterol-based cytofectins containing primary amino head groups, glycylcholesteryl formylhydrazide (MS10) and beta-alanylcholesterylformylhydrazide (MS11), have been prepared and incorporated into unilamellar cationic liposomes in equimolar amounts with dioleoylphosphatidylethanolamine (DOPE) as colipid. Stable lipoplexes were formed with pGL3 DNA which afforded protection to the DNA from serum nuclease digestion. Packing of the DNA was shown by ethidium displacement to be more effective in MS11 lipoplexes. High transfection levels in three human transformed epithelial cell lines HeLa (cervical), SNO (esophageal), HepG2 (hepatocyte-derived), and the murine fibroblast line NIH-3T3 were achieved by both lipoplexes at liposome: DNA ratios of 6:1 and 7:1 ((w)/(w)) corresponding to +/- charge ratios of 1.6:1 and 1.9:1. MS11 lipoplexes, in particular, afforded high transfection activities in the presence of fetal bovine serum.